Preparation and in vitro characterizations of cyclosporine A ocular nanostructured lipid carriers / 中国药学杂志

ABSTRACT

OBJECTIVE: To develop an appropriate nanostructured lipid carrier (CsA-NLC) for ocular drug delivery of cyclosporine A and its in vitro physicochemical properties and ocular irritation studies were investigated. METHODS: The melt-emulsification method was chosen to prepare CsA-NLC. The formulation was optimized by orthogonal design. The morphology of CsA-NLC was observed by transmission electron microscopy (TEM). The mean particle size and Zeta potential were measured by laser particle size analyzer. The state of drug in NLC was confirmed by DSC. Drug loading and encapsulation efficiency were determined by HPLC. Dialysis method at 34°C was employed to investigate the in vitro release of CsA-NLC. The topical ocular irritation study of CsA-NLC was made in rabbits. RESULTS: The obtained CsA- NLC was approximately spherical in shape with average particle size of (35.9 ± 0.21) nm and zeta potential of (- 13.9 ± 0.21) mV. The drug loading and encapsulation efficiency were (16.2 ± 0.09)% and (97.5 ± 0.58)%, respectively. The in vitro release of CsA-NLC was slowed down and fitted well single exponential distribution model. There was no irritation for CsA-NLC to rabbits eye. CONCLUSION: CsA-NLC with small particle sizes and high drug loading, slow release would be a promising nanocarrier for ocular drug delivery to improve drugs bioavailability. Copyright 2012 by the Chinese Pharmaceutical Association.